Construction of CF3‐containing Oxepino[2, 3‐c]pyrazole Motif via Sulfur Ylide‐mediated Annulation or Me2S involved One‐pot Reaction. Issue 11 (13th October 2021) - Yang, Kaichuan
Abstract: Base promoted [4+3] annulation of trifluoromethylpyrazole(TFPZ) derived α, β ‐unsaturated ketones with crotonate‐derived sulfur ylides provided a diverse set of CF3 ‐containing oxepino[2, 3‐ c ]pyrazole motif in good to excellent yields through a simple, mild and fast manner. Significantly, one‐pot strategy could be successfully applied to this transformation from available materials. Also, the utility of our versatile protocol was further demonstrated by gram‐scale reaction and useful derivation. Abstract : A diverse set of CF3 ‐containing oxepino[2, 3‐c]pyrazoles were obtained through direct [4+3] annulation or one‐pot strategy based on trifluoromethylpyrazole(TFPZ) derived α, β ‐unsaturated ketones.